RESUMO
OBJECTIVE: We aim to investigate the sonodynamic effect induced by hydroxyl acetylated curcumin (HAC) on THP-1 macrophages. METHODS: THP-1 derived macrophages (1 x 10(5) per milliliter) were cultured with HAC at a concentration of 5 µg/mL for 4 h and then exposed to pulse ultrasound treatment (0.5 W/cm2) for 5 min. Six hours later, cell viability analysis was performed with CCK-8 assay, apoptosis and necrosis analysis were detected with Annexin V/PI staining by flow cytometery. RESULTS: The cell viability of THP-1 macrophage decreased significantly in the group treated with the combination of HAC and ultrasound (P < 0.01), and HAC-SDT induced both apoptosis and necrosis in THP-1 macrophages, the apoptotic rate was higher than the necrotic rate with appropriate conditions, the maximum apoptosis/necrosis ratio was detected in sonodynamic therapy (SDT) group (P < 0.01). CONCLUSION: hAC-SDT was effective to induce THP-1 macrophages apoptosis.
Assuntos
Apoptose , Curcumina/farmacologia , Macrófagos/citologia , Necrose , Linhagem Celular , Sobrevivência Celular , Humanos , Macrófagos/efeitos dos fármacos , UltrassomRESUMO
A new ent-kaurane diterpenoid, 3α, 14ß, 16α-trihydroxy-ent-kaurane (1), together with seven known diterpenoids (2-8), was isolated from the leaves of Isodon japonica. Their structures were elucidated by spectroscopic methods, including 1D and 2D NMR experiments, IR, HR-ESI-MS and X-ray crystallographic analysis.
Assuntos
Diterpenos do Tipo Caurano/química , Isodon/química , Folhas de Planta/química , Espectroscopia de Ressonância MagnéticaRESUMO
Three new ENT-kaurane diterpenoids, glaucocalyxin H ( 1), glaucocalyxin I ( 2), and glaucocalyxin J ( 3), together with four known diterpenoids ( 4- 7), were isolated from the leaves of Isodon japonica Hara var. glaucocalyx. Their structures were elucidated by spectroscopic analysis, and the structures of compounds 2 and 3 were further confirmed by X-ray crystallographic analysis. Compounds 1, 4, and 5 were evaluated for their cytotoxicity IN VITRO against CE-1, U87, A-549, MCF-7, Hela, K-562, and HepG-2 human tumor cell lines. Compound 1 showed potent inhibitory activities against six tumor cell lines with IC (50) values ranging from 1.86-10.95 µM, and compounds 4 and 5 exhibited significant selective cytotoxicity on seven tumor cell lines.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/farmacologia , Isodon/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Bioensaio , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Folhas de Planta/química , Plantas Medicinais/químicaRESUMO
In the title compound, C(46)H(80)O(3), a natural ursane-type triperpenoid, four of the five six-membered rings adopt chair conformations; the fifth, which has a C=C double bond, adopts an approximate half-boat conformation. In the crystal, mol-ecules are linked by O-Hâ¯O hydrogen bonds, forming chains along [010].
